/ 
Instituto de Fisiologia Celular UNAM
Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosoma
Armando Gómez Puyou; Marieta Tuena Sangri; Ruy Pérez Montfort; Cabrera, N; Cerecetto, H; Gonzalez, M; Di Maio, R; Porcal, W; Lavaggi, ML; Lopez, GV; Merlino, A; Cabrera, M; Varela, J; Aguirre-Lopez, B; Alvarez, G;
Publication date: 2010
Journal: EUR J MED CHEM
Volume: 45
Issue: 12
Pages: 5767-5772
TEXT
Triosephosphate isomerase from Trypanosoma cruzi (TcTIM), an enzyme in the glycolytic pathway that exhibits high catalytic rates of glyceraldehyde-3-phosphate- and dihydroxyacetone-phosphate-isomerization only in its dimeric form, was screened against an in-house chemical library containing nearly 230 compounds belonging to different chemotypes. After secondary screening, twenty-six compounds from eight different chemotypes were identified as screening positives. Four compounds displayed selectivity for TcTIM over TIM from Homo sapiens and, concomitantly, in vitro activity against T cruzi. (C) 2010 Elsevier Masson SAS. All rights reserved.
Keywords: T. cruzi  TIM  Massive screening  Drug discovery  
Journal impact: 3.19
RANK
Todos los Artículos:
Marietta Tuena Sangri
A Ribosomal Misincorporation of Lys for Arg in Human Triosephosphate Isomerase Expressed in Escherichia coli Gives Rise to Two Protein Populations (2011)
-
Structural and biochemical characterization of a recombinant triosephosphate isomerase from Rhipicephalus (Boophilus) microplus (2011)
-
Structural basis of human triosephosphate isomerase deficiency: Mutation E104D is related to alterations of a conserved water network at the dimer int (2008)
-
Ver más artículos: Marietta Tuena Sangri
Todos los Artículos:
Ruy Pérez Montfort
Structural and biochemical characterization of a recombinant triosephosphate isomerase from Rhipicephalus (Boophilus) microplus (2011)
-
Identification of Amino Acids that Account for Long-Range Interactions in Two Triosephosphate Isomerases from Pathogenic Trypanosomes (2011)
-
Thermodynamic and Kinetic Destabilization of Triosephosphate Isomerase Resulting from the Mutation of Conserved and Non-conserved Cysteines (2011)
-
Ver más artículos: Ruy Pérez Montfort
Todos los Artículos:
Armando Gómez Puyou
Structural and biochemical characterization of a recombinant triosephosphate isomerase from Rhipicephalus (Boophilus) microplus (2011)
-
Identification of Amino Acids that Account for Long-Range Interactions in Two Triosephosphate Isomerases from Pathogenic Trypanosomes (2011)
-
A Ribosomal Misincorporation of Lys for Arg in Human Triosephosphate Isomerase Expressed in Escherichia coli Gives Rise to Two Protein Populations (2011)
-
Ver más artículos: Armando Gómez Puyou
Buscas a alguien?
-



-